Gene expression profiling of epothilone A-resistant cells

Novartis Found Symp. 2002:243:119-32; discussion 132-6, 180-5. doi: 10.1002/0470846356.ch9.

Abstract

In the current study, we isolated sublines of the human breast adenocarcinoma cell line MDA 435 that exhibited increasing resistance to epothilone A, a microtubule-stabilizing cytotoxic agent. The resistant cells did not express P glycoprotein or multidrug resistance-associated protein (MRP) which are known mediators of multidrug resistance (MDR). Two groups of epothilone A-resistant cells were selected: cells which exhibited low resistance to both epothilone A and Taxol, and cells which exhibit low resistance to Taxol but high resistance to epothilone A. cDNA microarrays of epothilone A-resistant and Taxol-resistant cells were utilized to further characterize epothilone A resistance. Hierarchical clustering of genes according to their levels of expression indicated that the majority of genes which were highly expressed in epothilone A-resistant cells but not in taxol-resistant MDR cells encode known interferon-inducible proteins. Genes whose expression increased with increasing epothilone A resistance include microtubule-associated GTPases, cytoskeletal proteins, cell signalling proteins and a drug metabolising enzyme. The majority of the genes that were repressed in both epothilone A- and Taxol-resistant cells encode proteins regulating cellular growth signalling mechanisms.

MeSH terms

  • Adenocarcinoma / genetics
  • Adenocarcinoma / pathology
  • Antineoplastic Agents / pharmacology*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology
  • Cytoskeletal Proteins / biosynthesis
  • Cytoskeletal Proteins / genetics
  • Drug Resistance, Neoplasm / genetics
  • Epothilones / pharmacology*
  • Female
  • GTP Phosphohydrolases / biosynthesis
  • GTP Phosphohydrolases / genetics
  • Gene Expression Profiling*
  • Gene Expression Regulation, Neoplastic* / drug effects
  • Growth Substances / biosynthesis
  • Growth Substances / genetics
  • HL-60 Cells / drug effects
  • Humans
  • Interferons / pharmacology
  • Male
  • Microtubules / drug effects
  • Neoplasm Proteins / biosynthesis
  • Neoplasm Proteins / genetics*
  • Neoplasm Proteins / physiology
  • Paclitaxel / pharmacology
  • Tumor Cells, Cultured / drug effects
  • Tumor Cells, Cultured / metabolism

Substances

  • Antineoplastic Agents
  • Cytoskeletal Proteins
  • Epothilones
  • Growth Substances
  • Neoplasm Proteins
  • epothilone A
  • Interferons
  • GTP Phosphohydrolases
  • Paclitaxel
  • epothilone B